Active substanceAmiodaroneAmiodarone
Similar drugsTo uncover
  • Amiodarone
    pills inwards 
  • Amiodarone
    concentrate in / in 
  • Amiodarone
    pills inwards 
    ALTAYVITAMINS, CJSC     Russia
  • Amiodarone
    concentrate in / in 
    ELLARA, LTD.     Russia
  • Amiodaron Belupo
    pills inwards 
  • Amiodarone Sandoz®
    pills inwards 
    Sandoz d.     Slovenia
  • Amiodarone-OBL
    pills inwards 
  • Amiodarone-Acry®
    pills inwards 
    AKRIKHIN HFK, JSC     Russia
  • Amiodarone-SZ
    pills inwards 
    NORTH STAR, CJSC     Russia
  • Amiocordin®
    solution in / in 
  • Amiocordin®
    pills inwards 
  • Vero-Amiodarone
    solution in / in 
    VEROPHARM SA     Russia
  • Cardiodarone®
    solution in / in 
    VALENTA PHARM, PAO     Russia
  • Cardiodarone®
    pills inwards 
    VALENTA PHARM, PAO     Russia
  • Cordarone®
    pills inwards 
  • Cordarone®
    solution in / in 
  • Dosage form: & nbsppills
    Composition:

    1 tablet contains: active ingredient: amiodarone hydrochloride 200.0 mg;

    auxiliary substances: lactose monohydrate 96.0 mg; cornstarch 60.0 mg; Povidone-K25 (viscosity of 1% aqueous solution - 1,163 - 1,200 Pas) 12,0 mg; magnesium stearate 4.6 mg; silicon dioxide colloidal 2,4 mg.

    Description:White, round biconvex tablets, with a risk on one side.
    Pharmacotherapeutic group:Antiarrhythmic drug
    ATX: & nbsp

    C.01.B.D.01   Amiodarone

    Pharmacodynamics:

    Amiodarone belongs to the third class of antiarrhythmic drugs (repolarization inhibitor). It has a unique mechanism of antiarrhythmic action, in addition to the properties of class III antiarrhythmics (potassium channel blockade), it has the effects of class I antiarrhythmics (sodium channel blockade), class IV antiarrhythmics (calcium channel blockade), and uncompetitive beta-blocking action. It also has antianginal, coronary-extending, alpha and beta-adrenergic blocking effects.

    Antiarrhythmic action is influenced by the electrophysiological

    myocardial processes; lengthens the action potential of cardiomyocytes (lengthens the interval QT), increasing the effective refractory period of the atria, ventricles, atrioventricular (AV) node, a bundle of His and Purkinje fibers, additional ways of conducting excitation, but does not affect the sharpness and amplitude of depolarization. Such an increase in the action potential associated exclusively with Phase 3 is a consequence of the slowing down of the outgoing current of potassium ions (Class III, V. Williams).

    By blocking the "fast" sodium channels, it has effects characteristic of class I antiarrhythmics. It inhibits the slow (diastolic) depolarization of the membrane of the cells of the sinus node, causing bradycardia, depresses AV conduction (effect of antiarrhythmics IV class). This effect is not antagonized by atropine. Antianginal effect is due to coronary and anti-adrenergic action. Reduces the need for myocardium in oxygen because of a moderate decrease in peripheral vascular resistance and a decrease in the heart rate. Increases coronary blood flow due to direct influence on the smooth muscles of the coronary arteries. Has a retarding effect on alpha and beta-adrenergic receptors of the cardiovascular system (without complete blockade). Reduces sensitivity to hyperstimulation of the sympathetic nervous system, resistance of coronary vessels; increases the energy reserves of the myocardium (by increasing the content of creatine sulfate, adenosine and glycogen).

    Reduces pressure in the aorta and peripheral resistance, contributing to maintaining a minute volume.

    Other properties: Does not have a significant inotropic effect on the myocardium, neither normal nor with heart failure. It is similar in its structure to thyroid hormones. The iodine content is about 37% of its molecular weight. Affects the exchange of thyroid hormones, inhibits the conversion of T4 to T3 (blockade of thyroxine-5-deiodinase) and blocks the seizure of these hormones by cardiocytes and hepatocytes, which leads to a weakening of the stimulating effect of thyroid hormones on the myocardium.

    The onset of action (even when using "loading" doses) - from 2-3 days to 2-3 months, the duration of the action varies from several weeks to months (determined in blood plasma for 9 months after discontinuation of its administration).

    It should be taken into account the possibility of maintaining the pharmacodynamic action of amiodarone within 10-30 days after its cancellation.

    Pharmacokinetics:

    Absorption slow and variable, bioavailability - 30-80% (mean value about 50%). After a single dose, the maximum concentration in the blood plasma is observed after 3-7 hours.

    The range of the therapeutic concentration of the drug in the blood plasma is 1-2.5 mg / l (but in determining the dose, one should also bear in mind the clinical picture). The time to reach a saturating dose in the blood serum from several days to several weeks (depending on the individual characteristics).

    Distribution.

    The volume of distribution is 60 liters, which indicates an intensive distribution in the tissue. Amiodarone - a molecule, which is characterized by a slow time of distribution throughout the body and a pronounced affinity to the tissues. Has a high affinity for adipose tissue and organs with good blood supply (concentration in fatty tissue tissue, liver, kidney, myocardium is higher than in blood plasma - respectively, in 300, 200, 50 and 34 times).

    Connection with blood plasma proteins 90% (62% with albumin, 33.5% with beta-lipoproteins). Penetrates through the blood-brain barrier and the placenta, is secreted with breast milk (25% of the dose received by the mother).

    Metabolized in the liver. The main metabolite, desethylamiodarone, is pharmacologically active and may increase the antiarrhythmic effect of the basic compound. It is also possible by deiodination (at a dose of 200 mg, about 6 mg of elemental iodine is released within 24 hours).With prolonged treatment, iodine concentrations can reach -60-80% of the concentrations of amiodarone. Is an inhibitor of isoenzymes CYP2C9, CYP2D6 and CYP3A4, CYP3A5, CYP3A7 in the liver.

    Given the capacity for cumulation and the associated large variability in pharmacokinetic parameters, data on the half-life period are contradictory.

    Excretion Amiodarone after oral administration is carried out in 2 phases: the initial period is 4-21 hours, in the second phase the half-life period is 25-110 days. After long oral administration, the average half-life is 40 days (this is important in choosing a dose, since it may be necessary, at least 1 month, to stabilize a new concentration of amiodarone in the blood plasma, while complete elimination may last up to 9 months).

    It is excreted with bile (85-95%), the kidneys are excreted less than 1% of the dose taken internally (therefore, due to the insignificant removal of the drug by the kidneys in patients with renal insufficiency, correction of the dose of amiodarone is not required).

    Amiodarone and its metabolites are not dialyzed.

    In view of the peculiarities of pharmacokinetics of amiodarone, the drug should be used in high loading doses.

    Indications:

    Relapse prevention

    Life-threatening ventricular arrhythmias, including ventricular tachycardia and ventricular fibrillation (treatment should be initiated in a hospital with careful cardiac monitoring).

    Nadzheludochkovyh paroxysmal tachycardia:

    documented attacks of recurrent persistent supraventricular paroxysmal tachycardia in patients with organic heart disease;

    documented attacks of recurrent persistent supraventricular paroxysmal tachycardia in patients without organic heart disease, when antiarrhythmic drugs of other classes are not effective, or there are contraindications to their use;

    documented attacks of recurrent persistent supraventricular paroxysmal tachycardia in patients with Wolff-Parkinson-White syndrome.

    Atrial fibrillation (atrial fibrillation) and atrial flutter.

    Preventing sudden arrhythmic death in high-risk patients

    Patients after a recent myocardial infarction, having more than 10 ventricular extrasystoles at 1 hour, clinical manifestations of chronic heart failure and a reduced fraction of the ventricular ejection (less than 40%).

    Amiodarone can be used in the treatment of rhythm disturbances in patients with coronary heart disease and / or impaired left ventricular function.

    Contraindications:

    Hypersensitivity to iodine, amiodarone or other components of the drug.

    Syndrome of weakness of the sinus node (sinus bradycardia and sinoatrial blockade, in the absence of an artificial pacemaker (the risk of "stopping" sinus node).

    Atrioventricular block II - IH degree, two- and three-beam blockade (in the absence of an artificial pacemaker pacemaker).

    Hypokalemia, hypomagnesemia.

    Thyroid dysfunction (hypothyroidism, hyperthyroidism).

    Interstitial lung diseases.

    Congenital or acquired lengthening interval QT.

    Pregnancy and lactation.

    Simultaneous reception with drugs that can lengthen the interval QT and cause the development of paroxysmal tachycardias, including polymorphic ventricular tachycardia such as "pirouette" (torsade de pointe): antiarrhythmics IA class (quinidine, disopyramide, procainamide),

    antiarrhythmic drugs of the III class (dofetilide, ibutilid, brethil tosylate); sotalol;
    other (not anti-arrhythmic) drugs, such as, beprideal; wincamine; some neuroleptics: phenothiazines (chlorpromazine, cyamemazine, levomepromazine, thioridazine, trifluoperazine, fluphenazine), benzamides (amisulpride, sultopride, sul-pyrid, tiapride, verialpyride), butyrophenones (droperidol, haloperidol), sertindole, pimozide; cisapride; tricyclic antidepressants; macrolide antibiotics (in particular erythromycin with intravenous administration, spiramycin); azoles; antimalarial drugs (quinine, chloroquine, mefloquine, halofantrine); pentamidine with parenteral administration; diphenamyl methyl sulfate; misolastine; astemizole, terfenadine; fluoroquinolones.

    Simultaneous administration of monoamine oxidase inhibitors (MAO).

    Age to 18 years (effectiveness and safety not established).

    Carefully:

    Caution should be used in patients with chronic heart failure (III-IV functional class by classification NYHA), severe arterial hypotension, collapse, cardiogenic shock, AV blockade of the I degree, hepatic insufficiency, bronchial asthma, lactose intolerance,deficiency of lactase or glucose-galactose malabsorption, in elderly patients (high risk of severe bradycardia).

    Pregnancy and lactation:

    Currently available clinical information is not sufficient to determine whether embryos can develop or develop in the first trimester of pregnancy.

    Since the fetal thyroid begins to bind iodine only from the 14th week of pregnancy (amenorrhea); then it is not expected that amiodarone will affect it if it is used earlier. Excess iodine in the use of the drug after this period can lead to the appearance of laboratory symptoms of hypothyroidism in a newborn or even to the formation of a clinically significant goiter in it.

    Due to the effect of the drug on the thyroid gland of the fetus, Amiodarone Sandoz® is not recommended for use during pregnancy, except in special cases when the expected benefit exceeds the risks (with life-threatening ventricular arrhythmias).

    Amiodarone is excreted in breast milk in a significant amount, so the drug is contraindicated for use during lactation.If it is necessary to prescribe the drug during this period, breastfeeding should be stopped.
    Dosing and Administration:

    The drug should be taken only as prescribed by the doctor!

    Tablets are taken orally, before eating, with plenty of water.

    Load ("saturating") dose

    In the hospital: the initial dose (divided into several doses) is 600-800 mg / day (up to a maximum dose of 1200 mg) until a total dose of 10 g is reached (usually within 8-10 days).

    Ambulatory: the initial dose divided into several doses is 600-800 mg / day until a total dose of 10 g is reached (usually within 10-14 days). Supportive dose. With maintenance treatment, the lowest effective dose is applied depending on the individual reaction of the patient and is usually 100-400 mg / day (1-2 tablets) in 1-2 divided doses.

    Due to the long half-life of the drug, you can take the drug every other day or take a break in taking the drug - 2 days a week.

    The average therapeutic single dose 200 mg.

    The average therapeutic daily dose 400 mg.

    Maximum single dose 400 mg.

    The maximum daily dose -1200 mg.

    Side effects:

    According to the World Health Organization (WHO), undesirable effects are classified according to their rate of development as follows: very common (> 1/10), common (> 1/100, <1/10), uncommon (> 1/1000, <1/100) rarely (> 1/10000, <1/1000) and very rarely (<1/10000); frequency is unknown (the frequency of occurrence of phenomena can not be determined on the basis of available data).

    From the side of the immune system the frequency is unknown: angioedema (Quincke's edema).

    From the cardiovascular system often: moderate bradycardia (dose-dependent); infrequently: sinoatrial and AV blockade of various degrees, proarrhythmic action up to sinus arrest (the emergence of new or aggravation of existing arrhythmias, including with cardiac arrest), in some cases asystole was observed; very rare bradycardia, stopping the sinus node (in patients with sinus node dysfunction and elderly patients), progression of chronic heart failure (with prolonged use), ventricular fibrillation / flutter; frequency unknown: ventricular tachycardia of the "pirouette" type.

    From the side of the digestive system very often: nausea, vomiting, loss of appetite, dullness or loss of taste, dysgeusia (metallic taste in the mouth),feeling of heaviness in the epigastrium, increased activity of an isolated "liver" enzymes (1,5-3 times higher than normal), usually moderate and reduces in dose reduction or even spontaneously; often: Acute toxic hepatitis with increased activity of "liver" transaminases and / or jaundice, including development of hepatic insufficiency, incl. with lethal outcome; very rarely: chronic hepatic insufficiency (pseudo-alcoholic hepatitis, cirrhosis), incl. with a lethal outcome, pancreatitis.

    On the part of the respiratory system often: interstitial or alveolar pneumonitis, allergic pneumonitis, bronchiolitis obliterans with pneumonia, incl. with a lethal outcome, pleurisy, pulmonary fibrosis; very rarely: bronchospasm in patients with severe respiratory failure (especially in patients with bronchial asthma), acute respiratory syndrome (distress syndrome), incl. with lethal outcome; pulmonary hemorrhage.

    From the senses very often: microcalcifications in the corneal epithelium, consisting of complex lipids, including lipofuscin (complaints on color appearance of ghosting or fuzziness of contours of objects in bright light), scotoma, macular degeneration, photosensitivity and degeneration of the cornea; rarely: optic neuritis / visual neuropathy.

    From the side of metabolism often: hypothyroidism, hyperthyroidism; very rarely: syndrome of impaired secretion of antidiuretic hormone.

    On the part of the skin is very often: photosensitivity; often: grayish or bluish skin pigmentation (with prolonged use, disappears after discontinuation of the drug); very rarely: erythema (with simultaneous radiotherapy), skin rash, exfoliative dermatitis (there is no connection with taking the drug), erythema multiforme and Stevens-Johnson syndrome, alopecia; frequency unknown: hives.

    From the side of the central nervous system often: tremor and other extrapyramidal symptoms, sleep disturbances, incl. "nightmarish" dreams; infrequent: peripheral neuropathy (sensorimotor, motor, mixed) and / or myopathy, usually reversible after drug withdrawal, dizziness; very rarely: cerebellar ataxia, benign intracranial hypertension (pseudotumour of the brain), headache. On the part of the blood and lymphatic system very rarely: thrombocytopenia, hemolytic or aplastic anemia, neutropenia, pancytopenia.Other often: weakness in the muscles; very rarely: peripheral edema, anaphylactic shock, epididymitis, impotence (connection with the drug is not established), myopathy, vasculitis, an increase in the concentration of creatinine in the blood plasma; frequency unknown: bone marrow granuloma.

    Overdose:

    Symptoms: sinus bradycardia, atrioventricular blockade, ventricular tachycardia / paroxysmal tachycardia of the pirouette type, increased symptoms of chronic heart failure, impaired liver function, cardiac arrest. Treatment: gastric lavage and administration of activated charcoal, if the drug is taken recently; symptomatic therapy (with bradycardia - beta-adrenostimulyatori or staging pacemaker, with tachycardia such as "pirouette" - in / in the introduction of magnesium salts or pacing). There is no specific antidote, hemodialysis is ineffective.

    Interaction:

    Contraindicated combinations (risk of developing polymorphic ventricular tachycardia such as "pirouette"): antiarrhythmic drugs IA class (quinidine, hydroquinidine, disopyramide, procainamide); III class (dofetilide, ibutilide, brethil tosylate); sotalol; others (not anti-arrhythmic drugs), such as beprideal; wincamine, some neuroleptics: phenothiazines (chlorpromazine, cyamemazine, levomepromazine, thioridazine, trifluoperazine, fluphenazine); benzamides (amisulpride, sultopride, sulpiride, tiapride, verialpride); butyrophenones (droperidolhaloperidol); sertindole; pimozide; tricyclic antidepressants (doxepin, maprotiline, amitriptyline); cisapride; macrolide antibiotics (erythromycin with intravenous administration, spiramycin, azithromycin, clarithromycin), cotrimoxazole; azoles; antimalarial drugs (quinine, chloroquine, mefloquine, halofantrine, lumefantrine); pentamidine (parenterally); diphenamyl methyl sulfate; misolastine; astemizole; terfenadine; fluoroquinolones (in t.ch. moxifloxacin); cimetidine; vasopressor amines: dobutamine, epinephrine, isoprenaline, norepinephrine; antiemetics: domperidone, ondansetron; decongestants: ephedrine, pseudoephedrine, phenylephrine, phenylpropanolamine; sympathomimetics / bronchodilators: salmeterol, salbutamol.

    Not recommended combinations: beta-adrenoblockers, blockers of "slow" calcium channels (verapamil, diltiazem) - the risk of violation of automatism (pronounced bradycardia) and conduction; laxatives stimulating peristalsis of the intestine - the risk of developing a ventricular tachycardia such as "pirouette" against the background of hypokalemia caused by laxatives; When combined with amiodarone, laxatives of other groups should be used.

    Combinations requiring use with caution: diuretics that cause hypokalemia, amphotericin (intravenously), systemic glucocorticosteroids, tetracosactide - risk of developing ventricular rhythm disturbances, incl. ventricular tachycardia of the "pirouette" type; procainamide - risk of side effects of procainamide (amiodarone increases the concentration of procainamide and its metabolite N-acetylprocainamide in blood plasma); anticoagulants of indirect action (warfarin) - amiodarone increases the concentration of warfarin in the blood plasma (risk of bleeding) by inhibiting the isoenzyme CYP2C9. Regular monitoring of prothrombin time and the international normalized ratio (MNO) and correction of anticoagulant doses both during therapy with amiodarone,and after its cancellation; cardiac glycosides - a violation of automatism (pronounced bradycardia) and AV conduction (increased digoxin concentration in blood plasma); esmolol - violation of contractility, automatism and conductivity (suppression compensatory reactions of the sympathetic nervous system).

    Clinical monitoring and monitoring of the electrocardiogram is required: phenytoin, fosphenytoin - the risk of developing neurological disorders (amiodarone increases the concentration of phenytoin in the blood plasma by inhibiting the isoenzyme CYP2C9); flecainide - amiodarone increases its concentration in the blood plasma (by inhibiting the isoenzyme CYP2D6); medicinal agents metabolized with the participation of the isoenzyme CYP3A4 (ciclosporin, fentanyl, lidocaine, tacrolimus, sildenafil, midazolam, triazolam, dihydroergotamine, ergotamine, inhibitors of HMG-CoA reductase (statins), incl. simvastatin) -amiodarone increases their concentration in the blood plasma (the risk of their toxicity and / or increased pharmacodynamic effects); orlistat reduces the concentration of amiodarone and its active metabolite in the blood plasma; clonidine, guanfacine, cholinesterase inhibitors (donepezil, galantamine, rivastigmine, tacrine, ambenonium chloride, pyridostigmine, neostigmine), pilocarpine - risk of development of severe bradycardia (cumulative effect); cimetidine, grapefruit juice slows the metabolism of amiodarone and increases its concentration in the blood plasma; medicaments for inhalation anesthesia - the risk of bradycardia (atropine-resistant), reducing blood pressure, conduction abnormalities, decrease cardiac output, acute respiratory distress syndrome, including with a fatal outcome, the development of which is associated with high concentrations of oxygen; radioactive iodine - amiodarone (contains in its composition iodine) can disrupt the absorption of radioactive iodine, which can distort the results of a radioisotope study of thyroid function; rifampicin and preparations of St. John's Wort (Hypericum Perforatum) (strong inducers of the isoenzyme CYP3A4) - reduce the concentration of amiodarone in the blood plasma; HIV protease inhibitors (inhibitors of the isoenzyme CYP3A4) -can increase the concentration of amiodarone in the blood plasma; clopidogrel - it is possible to reduce its concentration in the blood plasma; dextromethorphan (a substrate of isoenzymes CYP3A4 and CYP2D6) - it is possible to increase its concentration in the blood plasma (amiodarone inhibits the isoenzyme CYP2D6).

    Special instructions:

    Before starting therapy Amiodarone Sandoz® it is necessary to conduct an electrocardiographic study, evaluate the function of the thyroid gland (hormone concentration), and the concentration of electrolytes in the blood plasma, and conduct an ophthalmological examination on a regular basis.

    The frequency and severity of side effects depend on the dose of the drug Amiodarone Sandoz®, therefore, minimal effective maintenance doses should be used.

    During therapy Amiodarone Sandoz® should regularly monitor the electrocardiography (every 3 months) and the activity of "liver" transaminases and other indicators of liver function, as well as the function of the thyroid gland (including several months after discontinuation of the drug), lung X-ray (every 6 months ) and functional pulmonary tests. If there is a drug during treatment Amiodarone Sandoz®, dyspnea and dry cough with or without worsening of general condition (increased fatigue, increased body temperature), it is necessary to perform chest X-ray examination for possible development of interstitial pneumonitis. In case of its development the drug is canceled.With the early cancellation of the drug (with or without treatment with glucocorticosteroids), these phenomena are usually reversible. Clinical manifestations usually disappear after 3-4 weeks, the restoration of the radiographic pattern and lung function takes place more slowly (several months).

    Before conducting a surgical procedure, it is necessary to inform the anesthetist about taking the drug Amiodarone Sandoz® (risk of increased hemodynamic effect of general and local anesthetics).

    In patients receiving long-term treatment Amiodarone Sandoz® about heart rhythm disturbances reported cases of increased incidence of ventricular fibrillation and / or an increase in the threshold of operation of a pacemaker or an implanted defibrillator, which may reduce their effectiveness. Therefore, before and during treatment with the drug Amiodarone Sandoz® should regularly check the correctness of their functioning.

    Because of the prolongation of the repose period of the ventricles of the heart, the pharmacological action Amiodarone Sandoz® causes certain changes on the ECG: lengthening of the interval QT, QTc (corrected), possibly the appearance U waves. Allowable lengthening interval QT - no more than 450 ms or no more than 25% of the initial value. These changes are not a manifestation of the toxic effect of the drug, however, require monitoring to correct the dose and evaluate the possible proarhythmogenic effect.

    When developing AV grade II blockade, sinoatrial blockade or a two-beam intraventricular blockade, Amiodarone Sandoz® treatment should be discontinued. When AV blockade of the I degree, it is necessary to strengthen patient monitoring.

    If there is a visual impairment (blurred vision, reduced visual acuity), an ophthalmological examination, including examination of the fundus, should be performed. With the development of optic neuropathy or optic neuritis, treatment with the drug Amiodarone Sandoz® is discontinued (risk of blindness).

    With the development of peripheral sensorimotor neuropathy and / or myopathy drug Amiodarone Sandoz® is canceled and symptoms regress for several months (in some cases may not be completely reversible).

    Safety and effectiveness of the application Amiodarone Sandoz® in children is not established, the onset and duration of the effect in them may be less than in adults.

    A drug Amiodarone Sandoz® contains iodine, so it can influence the results of tests of accumulation of radioactive iodine in the thyroid gland.

    When taking the drug is recommended to avoid UV radiation (sun or solarium) or apply protective measures (for example, sunscreen).

    Effect on the ability to drive transp. cf. and fur:

    Because of the possible slowing of the reaction rate due to the development of headache, visual impairment, etc. side effects, it is recommended to use caution when practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

    Form release / dosage:

    Tablets 200 mg.

    Packaging:10 tablets are placed in a blister of PP / aluminum foil. For 2, 5, 6 or 10 blisters are placed in a cardboard box together with instructions for medical use.
    Storage conditions:

    At a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    2 years.

    Do not use after the expiration date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-000770
    Date of registration:29.09.2011
    Date of cancellation:2017-11-27
    The owner of the registration certificate:Sandoz d.Sandoz d. Slovenia
    Manufacturer: & nbsp
    Representation: & nbspSANDOZ SANDOZ Switzerland
    Information update date: & nbsp27.11.2017
    Illustrated instructions
      Instructions
      Up